1. Technical Field
The present invention relates to a non-androgenic steroidal chemical. More particularly, the invention relates to the chemical 1,4,6-androstatriene-3,17-dione (“ATD”) and its metabolites and analogs for therapeutic use in humans and animals as an anti-aromatase, testosteronegenic and anti-estrogenic compound.
2. Description of Related Art
Estrogens are vital to human growth, development, sexual differentiation and other functions. However, excess estrogen may lead to diseases or problems in women including: weight gain, fibrocystic breast disease, migraine headaches, menstrual disturbances, endometriosis and certain types of PMS. Men may experience infertility and gynecomastia with excess levels of estrogen.
The enzyme aromatase is required for the conversion of androgens into estrogens. Because of its action, aromatase has been the target of pharmaceutical therapies aimed at decreasing circulating levels of estrogen. Inhibitors of aromatase generally act by blocking the aromatization of endogenous androgens, such as testosterone, into estrogens. The effect is a decrease in levels of circulating estrogens and a concomitant increase in levels of circulating androgens. Modern cancer treatments may utilize aromatase inhibitors to combat tumors that depend on estrogen for growth. For instance, the growth of many breast cancers is promoted by estrogens. Most estrogen after menopause comes from areas outside of the ovaries by the action of aromatase, when the ovaries are no longer producing estrogen. Aromatase inhibitors may therefore be used to treat estrogen-dependent tumors after menopause. Aromatase inhibitors simply prevent or severely limit aromatizable androgens from being converted to estrogen. Moreover, aromatase inhibition may be an element in a myriad of other therapies including increasing endogenous androgen levels without a concomitant rise or even change in estrogen levels. What is needed is an improved inhibitor of the aromatase enzyme.
While aromatase inhibitors have been effectively used to decrease circulating levels of estrogen, currently available treatments have substantial room for improvement. Aromatase inhibitors include 4-hydroxyandrostenedione and FORMESTANE which are inherent anabolic compounds. Because of their compositions, they often have undesirable anabolic and androgenic effects. In contrast, 3-beta-hydroxyandrost-4-ene-6,17-dione (“3-OHAT”) and androst-4-ene-3,6,17-trione (AT) are non-androgenic compounds. But they may require frequent and high dosing because of their relatively low potency and rapid metabolization. Many aromatase inhibitors will cause a rise in endogenous androgen levels but also cause a precipitous and possibly unwanted decrease in endogenous estrogen levels when used in men. Because currently available aromatase inhibitors may have undesirable side-effects or lack adequate potency or are very expensive to manufacture currently or decrease endogenous estrogen levels too much in men, improved anti-aromatase compounds are needed.